01773nas a2200229   4500008004100000022001400041245019600055210006900251260000900320300001400329490000700343520089800350100002101248700002201269700002601291700002301317700001501340700001801355700001901373700002101392856013001413       2024                        eng d  a0022-326300a2-Pyridone-directed CuII-catalyzed general method of C(sp2)-H activation for C-S, C-Se, and C-N cross-coupling: easy access to aryl thioethers, selenide ethers, and sulfonamides and DFT study0 a2Pyridonedirected CuIIcatalyzed general method of Csp2H activati  cAPR   a6798-68120 v893 a<p>
	We have demonstrated N-substituted 2-pyridones as an N,O-directing group for selective C(sp(2))-H-activated thiolation, selenylation, and sulfonamidation of ortho C-H bonds of benzamides. This method utilizes a cost-effective Cu(II)-salt catalyst instead of precious metal catalysts, achieving high yields, including gram-scale synthesis and excellent functional group tolerance. We applied this protocol to access 30 different compounds with high yields, demonstrating thiolation of fluorine-substituted benzamides as well. Density functional theory (DFT) calculations support the mechanism, including acetate-supported concerted metalation deprotonation (CMD) steps and the unique role of dimethyl sulfoxide (DMSO) solvent. The facile synthesis of pharmaceutically important sulfonamides and other compounds highlights the method's potential in chemistry and medicinal chemistry.</p>
1 aPati, Tanmay, K.1 aMolla, Sabir, Ali1 aGhosh, Narendra, Nath1 aKundu, Mrinalkanti1 aAjarul, Sk1 aMaity, Pradip1 aKhamrai, Uttam1 aMaiti, Dilip, K.  uhttps://library.ncl.res.in/content/2-pyridone-directed-cuii-catalyzed-general-method-csp2-h-activation-c-s-c-se-and-c-n-cross02132nas a2200193   4500008004100000022001400041245010900055210006900164260000900233300001600242490000800258520143400266100001901700700001801719700002201737700003001759700001801789856013101807       2026                        eng d  a0002-786300aMild and site-selective nucleophilic C-H functionalization of pyridines via its stable N-alkylated salts0 aMild and siteselective nucleophilic CH functionalization of pyri  cJUN   a22931-229410 v1483 a<p>
	Direct, site-selective C-H functionalization of pyridines offers an efficient approach to both streamlined synthesis and late-stage modification of bioactive and functional molecules. Existing approaches to direct nucleophilic substitution typically rely on highly reactive nitrogen-activating groups, which limit nucleophile scope and functional group tolerance and often suffer from poor site selectivity. Although milder activating groups address some of these limitations, they generally require additional installation and removal steps. Herein, we report a mild and general strategy employing designed alkyl halide activators that enables one-pot, site-selective functionalization of pyridines with synthetically valuable yet challenging nucleophiles. This strategy allows, for the first time, direct pyridine functionalization with a broad range of phosphites and amines, in addition to methoxide and cyanide. The mild and redox-neutral reaction conditions are particularly well suited for late-stage functionalization (LSF) of pharmaceutically relevant molecules, enabling site-selective modification with both phosphites and amines. The rational design of the alkyl halide activators, together with careful analysis of side-product formation, reveals the delicate balance required for success with electronically diverse nucleophiles and suggests broader applicability of this C-H functionalization strategy.</p>
1 aBaral, Nilofar1 aSaikia, Pinku1 aMolla, Sabir, Ali1 aDewangan, Devendra, Kumar1 aMaity, Pradip  uhttps://library.ncl.res.in/content/mild-and-site-selective-nucleophilic-c-h-functionalization-pyridines-its-stable-n-alkylated